- LYSOPHOSPHATIDIC ACID RECEPTOR ANTAGONISTS
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Compounds, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds to treat, prevent or diagnose diseases, disorders, or conditions associated with one or more of the lysophosphatidic acid receptors are provided.
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Paragraph 0436
(2013/03/26)
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- Discovery of (+)-N-(3-aminopropyl)-N-[1-(5-benzyl-3-methyl-4-oxo-[1,2] thiazolo[5,4- d ]pyrimidin-6-yl)-2-methylpropyl]-4-methylbenzamide (AZD4877), a kinesin spindle protein inhibitor and potential anticancer agent
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Structure-activity relationship analysis identified (+)-N-(3-aminopropyl)- N-[1-(5-benzyl-3-methyl-4-oxo-[1,2]thiazolo[5,4-d]pyrimidin-6-yl) -2-methylpropyl]-4-methylbenzamide (AZD4877), from a series of novel kinesin spindle protein (KSP) inhibitors, as exhibiting both excellent biochemical potency and pharmaceutical properties suitable for clinical development. The selected compound arrested cells in mitosis leading to the formation of the monopolar spindle phenotype characteristic of KSP inhibition and induction of cellular death. A favorable pharmacokinetic profile and notable in vivo efficacy supported the selection of this compound as a clinical candidate for the treatment of cancer.
- Theoclitou, Maria-Elena,Aquila, Brian,Block, Michael H.,Brassil, Patrick J.,Castriotta, Lillian,Code, Erin,Collins, Michael P.,Davies, Audrey M.,Deegan, Tracy,Ezhuthachan, Jayachandran,Filla, Sandra,Freed, Ellen,Hu, Haiqing,Huszar, Dennis,Jayaraman, Muthusamy,Lawson, Deborah,Lewis, Paula M,Nadella, Murali V. P.,Oza, Vibha,Padmanilayam, Maniyan,Pontz, Timothy,Ronco, Lucienne,Russell, Daniel,Whitston, David,Zheng, Xiaolan
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supporting information; experimental part
p. 6734 - 6750
(2011/12/04)
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- Selected fused heterocyclics and uses thereof
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This invention relates to novel compounds having the structural formula (I) and to their pharmaceutical compositions and to their methods of use. These novel compounds provide a treatment or prophylaxis of cancer.
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Page/Page column 13; 21
(2008/06/13)
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- NOVEL FUSED HETEROCYCLES AND USES THEREOF
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This invention relates to novel compounds having the formula (I) (a chemical formula should be inserted here - please see paper copy enclosed herewith) m = 0, 1, 2 n = 0, 1 (I) wherein R1, R2, R3, R4, R5, R6, R7, R8 and R9 are as defined in the specification and to their pharmaceutical compositions and to their methods of use. These novel compounds provide a treatment or prophylaxis of cancer.
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Page 33; 63; 65; 70; 74; 79
(2008/06/13)
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- Ink compositions
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An ink comprising water, a water-dissipatable polymer and one or more dyes of Formula (1): wherein:R1 is H or a substituent;R2 and R3 are each independently optionally substituted alkyl, aryl or aralkyl, or R2 andR3 together with the carbon atom to which they are attached form an optionally substituted ring;R4 is H or optionally substituted alkyl, aryl or aralkyl; andD is an optionally substituted arylene group. Also claimed are the dyes of Formula (1), ink jet printing processes and cartridges containing the inks.
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